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  • 學位論文

奈米藥物的合成與研究

Synthetic Studies on Nanoprodrugs

指導教授 : 黃博瑞

摘要


金奈米前趨藥物製備的目的在於避免藥物副作用、改善口服藥物的身體可用率、提高親脂性或增加膜滲透性提高吸收率等。因此將藥物修飾成前趨藥物可以改善副作用提高吸收率及身體可用率,到達體內可經由適當反應轉變成具有藥效的形式,使藥效達到最大,並將負作用降到最小。 本研究擬將非類固醇消炎止痛藥ibuprofen修飾成含有硫醇基之醯胺類前趨藥(2-(4-isobutylphenyl)-N-[4-(4-mercaptobut-2-enyloxy)- phenyl]propionamide、2-(4-isobutyphenyl)-N-(5-mercaptophentyl) propionamide與2-(4-isobutylphenyl)-N-(6-mercaptohexyl)- propionamide),再利用self-assembled monolayer 方式,結合在奈米金球上,探討其物化性質。期待此類金奈米前趨藥物,藉由奈米金球尺寸的調控將可大大減輕副作用,提高吸收速率及身體可用率。

關鍵字

奈米藥物

並列摘要


The prodrug, which was combined with gold nanoparticles, could avoid the side effects of drugs, improve the bioavailability and increase the hydrophobicity and permeation to the cell membrane. Therefore; modification of the prodrug tends to exhibit the excellent efficiency and prevent from side effects. In this thesis, ibuprofen, belongs to the nonsteroidal anti-inflammatory drugs (NSAIDs), were modified to contain thiol group. (2-(4-Isobutyl- phenyl)-N-[4-(4-mercaptobut-2-enyloxy)phenyl]propionamide,2-(4-isobutyphenyl)-N-(5-mercaptophentyl)propionamide and 2-(4-Isobutyl- phenyl)-N-(6-mercaptohexyl)propionamide were synthesized for the prodrugs of ibuprofen. These compounds were combined with gold nanoparticles by self-assembled method and their physical properties were discussed. The modified prodrugs of ibuprofen that combined with gold nanoparticles will be expected to decrease the side effects and increase the bioavailability of drugs.

並列關鍵字

Nanoprodrugs

參考文獻


1. Wang,Y.Acc. Chem. Res.1991, 24, 133
2. Andres, R. P.; Bielefeld, J. P.; Henderson, J. I.; Jance, D. B.; Kolaguna, V. R.; Kubiak, C. P.; Mahoney, W. J.; Osifchin, R. G. Science 1996, 273, 1690
3. Sun, S.; Murray, C. B.; Weller, D.; Holrs, L.; Moser, A. Science
2000, 287, 1989
4. Black, C. T.; Murray, C. B.; Sandstrom, R. L.; Sun, S. Science

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